1.
Bioorg Med Chem Lett
; 20(11): 3436-40, 2010 Jun 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20434910
RESUMO
A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT(6) for antagonism.
Assuntos
Receptores de Serotonina/metabolismo , Ligantes , Modelos Moleculares , Mutagênese Sítio-Dirigida , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 17(12): 3504-7, 2007 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17485206
RESUMO
A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.